Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
18
|
pubmed:dateCreated |
1983-10-28
|
pubmed:abstractText |
Photolabile derivatives of D-Ala2-Leu5-enkephalin were prepared by synthetic procedures in which a 2-nitro-4-azidophenyl group is linked to the terminal carboxyl group of the enkephalin by means of an ethylenediamine or ethylenediamine beta-alanine spacer. These peptides bind to opiate receptors with nanomolar affinities and inhibit electrically stimulated contractions of the mouse vas deferens and adenylate cyclase activity of NG108-15 neuroblastoma x glioma hybrid cell membranes. Both inhibitions are reversed by the opiate antagonist naloxone. Photolysis of the ligands bound to rat brain membranes results in the loss of approximately 50% of the receptor sites. This decrease in receptor number is blocked by naloxone and requires light. A photolabile [3H]enkephalin derivative labels an equivalent number of sites under similar irradiation conditions.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
0021-9258
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
25
|
pubmed:volume |
258
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
10934-7
|
pubmed:dateRevised |
2003-11-14
|
pubmed:meshHeading |
pubmed-meshheading:6309823-Animals,
pubmed-meshheading:6309823-Biological Assay,
pubmed-meshheading:6309823-Brain,
pubmed-meshheading:6309823-Enkephalin, Leucine,
pubmed-meshheading:6309823-Enkephalin, Leucine-2-Alanine,
pubmed-meshheading:6309823-Male,
pubmed-meshheading:6309823-Mice,
pubmed-meshheading:6309823-Muscle Contraction,
pubmed-meshheading:6309823-Photolysis,
pubmed-meshheading:6309823-Rats,
pubmed-meshheading:6309823-Receptors, Opioid,
pubmed-meshheading:6309823-Vas Deferens
|
pubmed:year |
1983
|
pubmed:articleTitle |
Photolabile opioid derivatives of D-Ala2-Leu5-enkephalin and their interactions with the opiate receptor.
|
pubmed:publicationType |
Journal Article
|